Tazarotene

Melting point: 95-98°C

Boiling point: 499.8±45.0°C(Predicted)

Density: 1.22±0.1 g/cm3(Predicted)

Storage temp: 2-8℃

Solubility: DMSO: >15 mg/mL

Form: Solid

Color: White to Very Faintly Yellow

1.Cell Experiment

Solubility in DMSO: 50 mg/mL (142.26 mM; solubilized by ultrasound; hygroscopic DMSO significantly affects product solubility, so use freshly opened DMSO).

Solubility in H2O: < 0.1 mg/mL (insoluble)

Preparing Stock Solutions:

Prepare a stock solution in an appropriate solvent based on the product's solubility in different solvents. Once prepared, aliquot and store to avoid product loss due to repeated freeze-thaw cycles.

Stock solution storage and expiration date: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, use within 2 years; when stored at -20°C, use within 1 year.

2.Animal Experiment

Please choose the appropriate dissolution method according to your experimental animals and administration method.

For the following dissolution protocols, first prepare a clear stock solution in vitro, then add cosolvents in sequence:

—To ensure reliable experimental results, the clear stock solution can be stored appropriately according to storage conditions. For in vivo experiments, it is recommended that the working solution be prepared fresh and used the same day.

The percentages shown before the solvents below refer to the volume percentage of the solvent in the final solution. If precipitation or precipitation occurs during the preparation process, heating and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent in order: 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline.

Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear Solution

This protocol produces a clear solution of ≥ 2.5 mg/mL (saturation unknown).

For a 1 mL working solution, add 100 μL of the 25.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix thoroughly. Add 50 μL of Tween-80 to the solution and mix thoroughly. Then, add 450 μL of saline to bring the volume to 1 mL.

To prepare saline solution: Dissolve 0.9 g of sodium chloride in ddH₂O and dilute to 100 mL. This will yield a clear, transparent saline solution.

Protocol 2

Please add each solvent in the following order: 10% DMSO, 90% corn oil.

Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear solution

This protocol produces a clear solution of ≥ 2.5 mg/mL (saturation unknown). This protocol should be used for animal experiments with experimental durations exceeding two weeks.

For a 1 mL working solution, add 100 μL of the 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix thoroughly.

Following topical application, tazarotene undergoes esterase hydrolysis to form its active metabolite, tazarotenic acid. When treating acne tazarotene may be taken in conjunction with an oral antibiotic. Tazarotene has been shown in peer-reviewed double blinded studies to reduce: mottling and hyperpigmentation, sallowness, fine wrinkling and coarse wrinkling in sun damaged skin. Histological studies have shown that long term (greater than 1 year) use of Tazarotene is associated with a significant reduction in atypical melanocytes and keratocytes - cells considered to be precursors of skin cancer. Some studies have shown long term use of Tazarotene to be associated with increased collagen production and better organization of skin collagen bundles.

Although the exact mechanism of tazarotene action is not known, studies have shown that the active form of the drug (tazarotenic acid) binds to all three members of the retinoic acid receptor (RAR) family: RARa, RARb, and RARg, but shows relative selectivity for RARb, and RARg and may modify gene expression. It also has affinity for RXR receptors.